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Encequidar mesylate

Catalog No. T11578L   CAS 849675-87-2
Synonyms: HM30181 mesylate, HM30181A mesylate

Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.

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Encequidar mesylate Chemical Structure
Encequidar mesylate, CAS 849675-87-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
5 mg In stock $ 72.00
10 mg In stock $ 98.00
25 mg In stock $ 181.00
50 mg In stock $ 315.00
100 mg In stock $ 495.00
500 mg In stock $ 1,120.00
1 mL * 10 mM (in DMSO) In stock $ 86.00
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Purity: 99.67%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Encequidar mesylate (HM30181A mesylate) is a competitive P-glycoprotein inhibitor.
In vitro Administration of Encequidar at concentrations of 0.1 or 1 nM resulted in a reduction of cell survival by 20% and 42% upon exposure to 100 nM and 1000 nM of NSC 125973, respectively [2].
In vivo When administered simultaneously, Encequidar demonstrates increased plasma concentrations with the microcapsule formulation compared to the powder, showing notable differences from 1 to 2 hours. The microcapsule formulation achieves a 1.7-fold quicker Tmax and a 1.6-fold greater AUC value than the powder (2.5±0.6 vs. 4.3±0.9 hours; 107.7±20.1 vs. 64.3±18.0 h ng/mL), indicating faster and more efficient absorption. This enhanced absorption of Encequidar in microcapsule format is likely attributed to its improved aqueous solubility and dissolution rates, facilitated by the conversion from crystalline to amorphous form and the reduction in particle size [1].
Synonyms HM30181 mesylate, HM30181A mesylate
Molecular Weight 784.83
Formula C39H40N6O10S
CAS No. 849675-87-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (31.85 mM), Sonication is recommended.

TargetMolReferences and Literature

1. Kim JC, et al. Effect of HM30181 mesylate salt-loaded microcapsules on the oral absorption of NSC 125973 as a novel P-glycoprotein inhibitor. Int J Pharm. 2016 Jun 15;506(1-2):93-101. 2. Joo KM, et al. Response of brain specific microenvironment to P-glycoprotein inhibitor: an important factor determining therapeutic effect of P-glycoprotein inhibitor on brain metastatic tumors. Int J Oncol. 2008 Oct;33(4):705-12.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Bioactive Compound Library Ion Channel Inhibitor Library Neuronal Signaling Compound Library Clinical Compound Library NO PAINS Compound Library

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Keywords

Encequidar mesylate 849675-87-2 Membrane transporter/Ion channel Neuroscience P-gp HM30181A HM 30181 Mesylate HM30181 Mesylate HM 30181 HM30181 mesylate Encequidar Mesylate HM30181 MDR1 ABCB1 HM-30181 Mesylate inhibit CD243 P-glycoprotein Cluster of differentiation 243 HM-30181 Inhibitor HM30181A Mesylate Encequidar Pgp HM30181A mesylate Multidrug resistance protein 1 inhibitor

 

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